Tetrahydrofuran → ethyl (R)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carbonyl]-amino}-3-(5,6,7,8-tetrahydro-naphthalen-2-yl)-propionate

Participants

Reaction Steps

A mixture of 20 mL THF, 1.65 g (6.7 mmol) ethyl (R)-2-amino-3-(5,6,7,8-tetrahydro-naphthalen-2-yl)-propionate and 1.25 g (7.6 mmol) CDT was stirred for 1 h in the ice bath and for 1 h at RT. Then 1.70 g (6.9 mmol) 3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one was added and the mixture was refluxed for 3 h. The reaction mixture was evaporated down under reduced pressure, the residue combined with 15% K2CO3 solution, the precipitate was suction filtered and dried.

Provenance & Evidence